EP3947368A4 - Agents de dégradation de cdk2/5 et utilisations associées - Google Patents
Agents de dégradation de cdk2/5 et utilisations associées Download PDFInfo
- Publication number
- EP3947368A4 EP3947368A4 EP20782155.4A EP20782155A EP3947368A4 EP 3947368 A4 EP3947368 A4 EP 3947368A4 EP 20782155 A EP20782155 A EP 20782155A EP 3947368 A4 EP3947368 A4 EP 3947368A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- degraders
- cdk2
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962829302P | 2019-04-04 | 2019-04-04 | |
| US202062981334P | 2020-02-25 | 2020-02-25 | |
| PCT/US2020/026411 WO2020206137A1 (fr) | 2019-04-04 | 2020-04-02 | Agents de dégradation de cdk2/5 et utilisations associées |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EP3947368A1 EP3947368A1 (fr) | 2022-02-09 |
| EP3947368A4 true EP3947368A4 (fr) | 2023-01-04 |
| EP3947368B1 EP3947368B1 (fr) | 2025-09-03 |
Family
ID=72666983
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP20782155.4A Active EP3947368B1 (fr) | 2019-04-04 | 2020-04-02 | Composés bifonctionells comprennant un ligand cdk2/5, un lieur et un dégron qui s'attache a la ligase d'ubiquitin e3 pour le traitement du cancer |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US12466809B2 (fr) |
| EP (1) | EP3947368B1 (fr) |
| AU (1) | AU2020256220A1 (fr) |
| CA (1) | CA3130706A1 (fr) |
| WO (1) | WO2020206137A1 (fr) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3142351A1 (fr) | 2019-05-31 | 2020-12-03 | Ikena Oncology, Inc. | Inhibiteurs de tead et leurs utilisations |
| WO2020243423A1 (fr) | 2019-05-31 | 2020-12-03 | Ikena Oncology, Inc. | Inhibiteurs de tead et leurs utilisations |
| CN111285851A (zh) * | 2020-03-23 | 2020-06-16 | 沈阳药科大学 | 靶向降解黏着斑激酶的化合物及其在医药上的应用 |
| WO2022120355A1 (fr) * | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Agents de dégradation de tead et leurs utilisations |
| US20250018049A1 (en) * | 2020-12-22 | 2025-01-16 | Nikang Therapeutics, Inc. | Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway |
| JP2024504932A (ja) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス， インコーポレイテッド | イソインドリノン化合物 |
| CA3217792A1 (fr) * | 2021-05-07 | 2022-11-10 | Kymera Therapeutics, Inc | Agents de degradation de cdk2 et leurs utilisations |
| WO2023006097A1 (fr) * | 2021-07-30 | 2023-02-02 | 海创药业股份有限公司 | Composé hétérocyclique chimère bifonctionnel et son utilisation en tant qu'agent de dégradation du récepteur des androgènes |
| WO2023069720A1 (fr) * | 2021-10-22 | 2023-04-27 | Monte Rosa Therapeutics, Inc. | Composés qui assurent la médiation de la dégradation de protéines et leurs procédés d'utilisation |
| WO2023069700A1 (fr) * | 2021-10-22 | 2023-04-27 | Monte Rosa Therapeutics, Inc. | Composés qui assurent la médiation de la dégradation de protéines et leurs procédés d'utilisation |
| WO2023143482A1 (fr) * | 2022-01-29 | 2023-08-03 | 上海辉启生物医药科技有限公司 | Composé ou sel de 2-aminopyrimidine, son procédé de préparation et son utilisation |
| WO2023239629A1 (fr) * | 2022-06-06 | 2023-12-14 | Plexium, Inc. | Composés et compositions pharmaceutiques qui dégradent cdk2 |
| CN119630644A (zh) * | 2022-06-21 | 2025-03-14 | 霖康疗法公司 | 用于经由泛素蛋白酶体途径降解细胞周期蛋白依赖性激酶2的含有嘧啶衍生物的双功能化合物 |
| WO2023250029A1 (fr) * | 2022-06-22 | 2023-12-28 | Nikang Therapeutics, Inc. | Composés bifonctionnels contenant des dérivés de pyrimidine substitués pour dégrader la kinase 2 dépendante des cyclines par l'intermédiaire d'une voie ubiquitine-protéasome |
| IL319254A (en) * | 2022-09-02 | 2025-04-01 | Auron Therapeutics Inc | History of Pyridazinone as KAT2 inhibitors for the treatment of proliferative disorders |
| WO2024054602A1 (fr) * | 2022-09-08 | 2024-03-14 | Halda Therapeutics Opco, Inc. | Composés hétérobifonctionnels et méthodes de traitement de maladie |
| WO2024092039A1 (fr) * | 2022-10-26 | 2024-05-02 | Monte Rosa Therapeutics, Inc. | Composés qui médient la dégradation des protéines et leurs procédés d'utilisation |
| IL320316A (en) * | 2022-11-11 | 2025-06-01 | Nikang Therapeutics Inc | Bifunctional compounds containing pyrimidine derivatives with substitutions at positions 2 and 5, for degradation of cyclin-dependent kinase 2 (CDK2) via the ubiquitin-proteasome pathway |
| TW202448467A (zh) * | 2023-04-20 | 2024-12-16 | 美商奧榮醫療公司 | 靶記細胞狀態之技術 |
| WO2025090727A1 (fr) * | 2023-10-25 | 2025-05-01 | Monte Rosa Therapeutics, Inc. | Composés qui assurent la médiation de la dégradation de protéines et leurs méthodes d'utilisation |
| WO2025117981A1 (fr) * | 2023-12-02 | 2025-06-05 | Nikang Therapeutics, Inc. | Composés bifonctionnels contenant des dérivés de pyrimidine 2,5-substitués pour dégrader la kinase 2 dépendante de la cycline par l'intermédiaire d'un système ubiquitine/protéasome |
| WO2025137385A1 (fr) * | 2023-12-20 | 2025-06-26 | Nikang Therapeutics, Inc. | Composés bifonctionnels contenant des dérivés de pyrido[2,3-d]pyrimidin-7(8h)-one pour dégrader la kinase cycline-dépendante 2 et la kinase cycline-dépendante 4 par l'intermédiaire d'une voie ubiquitine-protéasome |
| WO2025137391A1 (fr) * | 2023-12-20 | 2025-06-26 | Nikang Therapeutics, Inc. | Composés bifonctionnels contenant des dérivés de pyrido[2,3-d]pyrimidin-7(8h)-one permettant de dégrader la kinase 4 dépendante des cyclines par l'intermédiaire de la voie ubiquitine-protéasome |
| WO2025137393A1 (fr) * | 2023-12-20 | 2025-06-26 | Nikang Therapeutics, Inc. | Composés bifonctionnels contenant des dérivés de pyrido[2,3-d]pyrimidin-7(8h)-one pour la dégradation de kinases dépendantes des cyclines 2, 4 et 6 par l'intermédiaire de la voie ubiquitine-protéasome |
| WO2025212828A1 (fr) * | 2024-04-03 | 2025-10-09 | Nikang Therapeutics, Inc. | Composés bifonctionnels contenant des dérivés de pyrimidine 2,5-substitués pour dégrader la kinase cycline-dépendante 2 et la kinase cycline-dépendante 4 par l'intermédiaire de la voie ubiquitine-protéasome |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003076437A1 (fr) * | 2002-03-11 | 2003-09-18 | Schering Aktiengesellschaft | 2-heteroaryle-pyrimidines inhibitrices de la kinase dependante des cyclines, leur production et leur utilisation comme medicaments |
| WO2006034872A1 (fr) * | 2004-09-29 | 2006-04-06 | Bayer Schering Pharma Aktiengesellschaft | 2-anilinopyrimidine substituee utilisee en tant que kinase a cycle cellulaire ou recepteur de la tyrosine kinase, leur production et leur utilisation en tant que medicament |
| WO2017185034A1 (fr) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Dégradation de la kinase 8 cycline-dépendante (cdk8) par conjugaison d'inhibiteurs de cdk8 avec un ligand de type ligase e3 et leurs procédés d'utilisation |
| WO2017185023A1 (fr) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Dégradation de la kinase 9 cycline-dépendante (cdk9) par conjugaison d'inhibiteurs de cdk9 avec un ligand de type ligase e3 et leurs procédés d'utilisation |
| WO2017197055A1 (fr) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Dégronimères hétérocycliques pour la dégradation de protéines cibles |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| PL367130A1 (en) | 2001-05-29 | 2005-02-21 | Schering Aktiengesellschaft | Cdk inhibiting pyrimidines, production thereof and their use as medicaments |
| US7968569B2 (en) | 2002-05-17 | 2011-06-28 | Celgene Corporation | Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione |
| PE20110220A1 (es) | 2006-08-02 | 2011-04-11 | Novartis Ag | DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS |
| EA017797B1 (ru) | 2007-04-13 | 2013-03-29 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Бициклические диазомиметики smac, способы их получения, их применения, содержащие их фармацевтические композиции и набор, содержащий указанные композиции |
| WO2013039854A1 (fr) | 2011-09-15 | 2013-03-21 | Merck Sharp & Dohme Corp. | Compositions et méthodes de traitement du cancer |
| GB201218864D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218862D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| AU2014312261A1 (en) * | 2013-08-28 | 2016-03-10 | Novartis Ag | Combination of an ALK inhibitor and a CDK inhibitor for the treatment of cell proliferative diseases |
| RU2696310C1 (ru) | 2013-12-20 | 2019-08-01 | Астекс Терапьютикс Лимитед | Бициклические гетероциклические соединения и их применение в терапии |
| EP3669881B1 (fr) | 2014-01-28 | 2022-03-30 | Buck Institute for Research on Aging | Compositions pour leur utilisation pour traiter les maladies et les troubles oculaires associés à la sénescence |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| EP3256470B1 (fr) | 2014-12-23 | 2023-07-26 | Dana-Farber Cancer Institute, Inc. | Procédés pour induire la dégradation ciblée de protéines par des molécules bifonctionnelles |
| EP3337476A4 (fr) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Composés et procédés pour la dégradation ciblée de protéines contenant un bromodomaine |
| WO2017079267A1 (fr) | 2015-11-02 | 2017-05-11 | Yale University | Composés chimères de ciblage de protéolyse et procédés de préparation et d'utilisation de ceux-ci |
| JP6921115B2 (ja) | 2016-04-22 | 2021-08-18 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | サイクリン依存性キナーゼ４／６（ｃｄｋ４／６）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ４／６の分解および使用法 |
| WO2017197046A1 (fr) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Dégronimères de type glutarimide liés au carbone c3 pour la dégradation de protéines cibles |
| WO2017197051A1 (fr) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Dégronimères de c3-glutarimide liés à une amine pour la dégradation de protéines cibles |
| EP3454862B1 (fr) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Dégronimères spirocycliques pour la dégradation de protéines cibles |
| WO2017197056A1 (fr) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Dégronimères ciblant un bromodomaine pour la dégradation de protéines cibles |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
-
2020
- 2020-04-02 AU AU2020256220A patent/AU2020256220A1/en active Pending
- 2020-04-02 WO PCT/US2020/026411 patent/WO2020206137A1/fr not_active Ceased
- 2020-04-02 US US17/442,923 patent/US12466809B2/en active Active
- 2020-04-02 EP EP20782155.4A patent/EP3947368B1/fr active Active
- 2020-04-02 CA CA3130706A patent/CA3130706A1/fr active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003076437A1 (fr) * | 2002-03-11 | 2003-09-18 | Schering Aktiengesellschaft | 2-heteroaryle-pyrimidines inhibitrices de la kinase dependante des cyclines, leur production et leur utilisation comme medicaments |
| WO2006034872A1 (fr) * | 2004-09-29 | 2006-04-06 | Bayer Schering Pharma Aktiengesellschaft | 2-anilinopyrimidine substituee utilisee en tant que kinase a cycle cellulaire ou recepteur de la tyrosine kinase, leur production et leur utilisation en tant que medicament |
| WO2017185034A1 (fr) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Dégradation de la kinase 8 cycline-dépendante (cdk8) par conjugaison d'inhibiteurs de cdk8 avec un ligand de type ligase e3 et leurs procédés d'utilisation |
| WO2017185023A1 (fr) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Dégradation de la kinase 9 cycline-dépendante (cdk9) par conjugaison d'inhibiteurs de cdk9 avec un ligand de type ligase e3 et leurs procédés d'utilisation |
| WO2017197055A1 (fr) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Dégronimères hétérocycliques pour la dégradation de protéines cibles |
Non-Patent Citations (2)
| Title |
|---|
| L�CKING ULRICH ET AL: "The Lab Oddity Prevails: Discovery of Pan-CDK Inhibitor ( R )- S -Cyclopropyl- S -(4-{[4-{[(1 R ,2 R )-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY?1000394) for the Treatment of Cancer", CHEMMEDCHEM COMMUNICATIONS, vol. 8, no. 7, 13 May 2013 (2013-05-13), DE, pages 1067 - 1085, XP055953788, ISSN: 1860-7179, DOI: 10.1002/cmdc.201300096 * |
| See also references of WO2020206137A1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2020256220A1 (en) | 2021-09-16 |
| EP3947368B1 (fr) | 2025-09-03 |
| WO2020206137A1 (fr) | 2020-10-08 |
| US20220153722A1 (en) | 2022-05-19 |
| US12466809B2 (en) | 2025-11-11 |
| EP3947368A1 (fr) | 2022-02-09 |
| CA3130706A1 (fr) | 2020-10-08 |
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